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Topical compositions for treatment of excessive sweating and methods of use thereof

一种组合物、化合物的技术，应用在药物组合、医药配方、梳妆用配制品等方向，能够解决未满足医疗需求等问题

Inactive Publication Date: 2016-05-04
GLAXOSMITHKLINE INTPROP DEV LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, identification of sweat glands that can be directly delivered by topical dermal administration to the axillae and palms (which have a larger amount of stratum corneum and may have higher barrier properties [Ya-Xian et al., ArchDermatolRes 1999; 291:555-559]) Potent, broadly active muscarinic acetylcholine receptor antagonists remain an unmet medical need

Method used

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  • Topical compositions for treatment of excessive sweating and methods of use thereof
  • Topical compositions for treatment of excessive sweating and methods of use thereof
  • Topical compositions for treatment of excessive sweating and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0240] Embodiment 1: pharmaceutical composition

[0241] The following compositions were prepared as indicated in the table below.

[0242] Table 1:

[0243]

[0244]

[0245] Formulation Nos. 1, 3, 4, 6, and 8 (solutions) were prepared by adding each solvent shown in Table 1 to a mixing vessel while stirring. Uclidinium was then added to the mixing vessel while stirring to obtain the desired solution formulation.

[0246] Formulation Nos. 2, 5, 7, 9 and 10 (gels) were prepared by adding each solvent shown in Table 1 to a mixing vessel while stirring. The umeclidinium is then added to the mixing vessel while stirring, followed by the addition of the hydroxypropyl cellulose to obtain the desired gel formulation.

[0247]The following additional formulations were also prepared to measure the viscosity of gel formulations according to the invention with different levels of gelling agent (0, 1%, 1.5% and 2% Klucel-MF):

[0248] Table 2:

[0249]

[0250]

[0251] ...

Embodiment 2

[0253] Example 2 - In Vitro Skin Penetration Study

[0254] The topical pharmaceutical composition described in Example 1 was subjected to an in vitro skin penetration study to measure skin flux. Use the following method:

[0255] Methods and Materials

[0256] Full thickness human skin was obtained from the patient via abdominoplasty at a local hospital. Immediately after collection the skin was transferred to a plastic container with phosphate buffered saline (PBS) and kept at 4°C for shipment. Once at the laboratory, subcutaneous fat is removed from the skin sample. Full-thickness skin was then placed on a block of high-density foam and harvested to a thickness of 500 μm using an Electro-Dermatome. The split thickness skin was then spread on aluminum foil and placed in a water impermeable plastic bag. The air is removed and the bag is heat sealed. Samples were stored at -80°C until the time of experiment. Previous experiments have shown that skin samples can be pre...

Embodiment 3

[0276] Example 3-in vitro skin penetration study (umeclidinium versus glycopyrronium bromide)

[0277] The in vitro study investigated the skin distribution (epidermal / dermal) and in vitro skin flux of the active ingredient delivered from (i) formulation number 1 shown in Table 1 containing 2.2% umeclidinium bromide and (ii) containing 2 % Glycopyrronium Bromide Comparative Formulation.

[0278] After administration of a single limited topical dose of umeclidinium bromide or glycopyrronium bromide on isolated human skin at 6 hours, the median value of the molar ratio of glycopyrronium bromide to umeclidinium bromide (after correcting for dose differences) was ( range) was 1.5 (0.4-5.8) in the epidermis and 1.2 (0.3-4.3) in the dermis. Thus, the amount of umeclidinium delivered to the dermis was of the same order (but on average slightly lower) than the amount of glycopyrronium bromide delivered to the dermis, based on normalized molar doses.

[0279] Following a single lim...

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PUM

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Abstract

The present invention provides for 4-[hydroxy(diphenyl)methyl]-1-{2- [(phenylmethyl)oxy]ethyl}-1-azoniabicyclo[2.2.2]octane and a pharmaceutically acceptable anion thereof for use in the topical treatment or prophylaxis of excessive sweating, and compositions containing these ingredients.

Description

technical field [0001] The present invention relates to topical pharmaceutical compositions for the treatment of excessive sweating, and methods of use thereof. Background technique [0002] Hyperhidrosis is a condition affecting approximately 3.0% of the US population and is defined as excessive sweating beyond that required to maintain the body's normal thermoregulatory physiology [Strutton et al., J Am Acad Dermatol. 2004; 51:241-248]. Primary hyperhidrosis (excessive sweating with no other explanation) is localized (small area) and can affect the armpits (underarms), palms, soles of feet, face, groin, trunk, and thighs. Secondary hyperhidrosis can be localized or generalized (whole body), and result from any number of medical conditions, including endocrine, metabolic, neurologic and cardiovascular disorders, and from drug use. [0003] As mentioned above, the most active areas of sweating include the hands, feet, armpits, and groin area. Excessive sweating is localize...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61P17/00A61Q15/00
CPCA61K31/439A61P17/00A61K8/39A61K8/4926A61K8/345A61Q15/00A61P25/02A61K2800/10A61K2800/74
Inventor T.X.佩内-杜米特雷斯库E.K.赫西M.G.拉姆J.莱恩L.卢佩诺克M.R.卢克L.L.桑托斯V.D.施米思
Owner GLAXOSMITHKLINE INTPROP DEV LTD
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